公开(公告)号：EP2685828A4

公开(公告)日：2014-08-13

申请号：EP12757995

申请日：2012-03-14

申请人： MERCK SHARP & DOHME

发明人： NAIR ANILKUMAR G ,  DUCA JOSE S ,  DWYER MICHAEL P ,  KOZLOWSKI JOSEPH A ,  ROSENBLUM STUART B

IPC分类号： A01N43/64 ,  A61K31/41 ,  C07D209/52 ,  C07D401/08 ,  C07D403/06 ,  C07D403/08 ,  C07D405/04 ,  C07D405/08 ,  C07D409/08 ,  C07D413/04 ,  C07D417/04 ,  C07D417/08 ,  C07D471/04 ,  C07D493/14

CPC分类号： C07D209/52 ,  C07D401/06 ,  C07D401/08 ,  C07D401/14 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/08 ,  C07D409/04 ,  C07D409/08 ,  C07D409/14 ,  C07D413/04 ,  C07D417/08 ,  C07D471/04

公开(公告)号：EP2736883A1

公开(公告)日：2014-06-04

申请号：EP12748083.8

申请日：2012-07-26

申请人： Karyopharm Therapeutics, Inc.

发明人： SANDANAYAKA, Vincent, P. ,  SHACHAM, Sharon ,  KAUFFMAN, Michael ,  SHECHTER, Sharon ,  MCCAULEY, Dilara ,  LANDESMAN, Yosef ,  SENAPEDIS, William ,  SAINT-MARTIN, Jean-Richard

IPC分类号： C07D213/50 ,  C07D401/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/08 ,  C07D403/12 ,  C07D413/12 ,  C07D487/10 ,  A61K31/4196 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/421 ,  A61K31/506 ,  A61K31/497 ,  A61K31/407

CPC分类号： C07D487/10 ,  C07D213/50 ,  C07D401/06 ,  C07D401/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/12

摘要： The invention generally relates to nuclear transport modulators, e.g CRM1 inhibitors, and more particularly to a compound represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula (I), or a pharmaceutically acceptable salt or composition thereof, e.g, in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.

摘要翻译： 或其药学上可接受的盐，其中变量如本文所定义和描述。 本发明还包括结构式I的化合物或其药学上可接受的盐或组合物的合成和用途，例如用于治疗，调节和/或预防与CRM1活性相关的生理条件。

公开(公告)号：EP2685828A1

公开(公告)日：2014-01-22

申请号：EP12757995.1

申请日：2012-03-14

申请人： Merck Sharp & Dohme Corp.

发明人： NAIR, Anilkumar, G. ,  DUCA, Jose, S. ,  DWYER, Michael, P. ,  KOZLOWSKI, JOseph, A. ,  ROSENBLUM, Stuart, B.

IPC分类号： A01N43/64 ,  A61K31/41

CPC分类号： C07D209/52 ,  C07D401/06 ,  C07D401/08 ,  C07D401/14 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/08 ,  C07D409/04 ,  C07D409/08 ,  C07D409/14 ,  C07D413/04 ,  C07D417/08 ,  C07D471/04

摘要： Disclosed are CCR2 antagonists of Formula (I) or pharmaceutically acceptable thereof, wherein R1, L1 and A are defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compounds, and compositions to treat diseases or disorders associated with CCR2 activity.

公开(公告)号：EP2660241A2

公开(公告)日：2013-11-06

申请号：EP13179069.3

申请日：2011-12-16

申请人： BioMarin Pharmaceutical Inc.

发明人： Chu, Daniel ,  Wang, Bing ,  Ye, Tao

IPC分类号： C07D401/08 ,  C07D403/08 ,  C07D405/08 ,  C07D413/08 ,  C07D471/04 ,  C07J43/00 ,  C07J61/00 ,  C07J63/00 ,  C07J73/00 ,  A61P5/26 ,  A61P5/42 ,  A61P5/46 ,  A61P35/00 ,  A61K31/56

CPC分类号： C07J73/008 ,  C07D401/08 ,  C07D403/08 ,  C07D405/08 ,  C07D413/08 ,  C07D471/04 ,  C07J1/0011 ,  C07J13/005 ,  C07J21/005 ,  C07J31/006 ,  C07J43/003 ,  C07J61/00 ,  C07J63/002 ,  C07J73/003 ,  C07J73/005

摘要： Provided herein are inhibitors of CYP11B, CYP17, and/or CYP21 enzymes of Formula Z, IX, X, XI, XII, XIII, XIV, XV, XVI, or XVII. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.

摘要翻译： 本文提供了式Z，IX，X，XI，XII，XIII，XIV，XV，XVI或XVII的CYP11B，CYP17和/或CYP21酶的抑制剂。 本文还描述了包含本文所述的至少一种化合物和本文所述的化合物或药物组合物用于治疗雄激素依赖性疾病，病症和病症的药物组合物。

公开(公告)号：EP2655326A1

公开(公告)日：2013-10-30

申请号：EP11802917.2

申请日：2011-12-19

申请人： Novartis AG

发明人： CARCACHE, David ,  GASPARINI, Fabrizio ,  KOLLER, Manuel ,  OFNER, Silvio ,  ORAIN, David ,  RENAUD, Johanne

IPC分类号： C07D209/08 ,  C07D401/06 ,  C07D417/06 ,  A61K31/404 ,  A61K31/427 ,  A61K31/4439 ,  A61P25/00 ,  A61P13/02 ,  A61P1/00

CPC分类号： C07D209/08 ,  A61K31/403 ,  A61K31/427 ,  A61K31/4439 ,  A61K45/06 ,  C07D401/06 ,  C07D401/08 ,  C07D417/06 ,  C07D417/08

摘要： The invention relates to compound of the formula (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.

公开(公告)号：EP2205083B1

公开(公告)日：2013-07-17

申请号：EP08835246.3

申请日：2008-09-30

申请人： Merck Sharp & Dohme Corp. ,  Neuromed Pharmaceuticals Ltd.

发明人： CHAKRAVARTY, Prasun, K. ,  DING, Yanbing ,  DUFFY, Joseph, L. ,  PAJOUHESH, Hassan ,  SHAO, Pengcheng Patrick ,  TYAGARAJAN, Sriram ,  YE, Feng

IPC分类号： A01N43/40 ,  A61K31/445

CPC分类号： C07D211/24 ,  C07D205/04 ,  C07D207/08 ,  C07D211/98 ,  C07D401/06 ,  C07D401/08 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D473/04 ,  C07D487/04

公开(公告)号：EP1751149B1

公开(公告)日：2012-06-06

申请号：EP05743943.2

申请日：2005-04-29

申请人： Abbott Laboratories

发明人： ALTENBACH, Robert, J. ,  BLACK, Lawrence, A. ,  CHANG, Sou-jen ,  COWART, Marlon, D. ,  FAGHIH, Ramin ,  GFESSER, Gregory, A. ,  KU, Yi-yin ,  LIU, Huaqing ,  LUKIN, Kirill, A. ,  NERSESIAN, Diana, L. ,  PU, Yu-ming ,  CURTIS, Michael, P.

IPC分类号： C07D401/08 ,  C07D417/14 ,  C07D401/04 ,  C07D417/04 ,  C07D413/04 ,  C07D409/14 ,  C07D215/12 ,  C07D401/14 ,  A61K31/4709 ,  A61P25/28 ,  A61P25/00 ,  C07D413/14

CPC分类号： C07D215/12 ,  C07D401/04 ,  C07D401/08 ,  C07D401/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

摘要： Compounds of formula (I) wherein R1 or R2 is an aromatic or non-aromatic ring directly joined or joined by a linker, as represented by L2 and L3, to a heteroaromatic core, and X, X', Y, Y', Z, Z', R1, R2, R3, R3a, R3b, R4, R5, L, L2, and L3 are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

公开(公告)号：EP2185540B1

公开(公告)日：2011-07-20

申请号：EP08786547.3

申请日：2008-07-29

申请人： F. Hoffmann-La Roche AG

发明人： JABLONSKI, Philippe ,  KAWASAKI, Kenichi ,  KNUST, Henner ,  LIMBERG, Anja ,  NETTEKOVEN, Matthias ,  RATNI, Hasane ,  RIEMER, Claus ,  WU, Xihan

IPC分类号： C07D401/08 ,  C07D401/06

CPC分类号： C07D401/06 ,  C07D401/08

摘要： The invention relates to a compound of general formula (I) wherein Ar1 is aryl or a five or six membered heteroaryl; Ar2 is aryl or a five or six membered heteroaryl; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, S-lower alkyl, -S(O)2-lower alkyl, -S(O)2-di-lower alkyl amino, -(CH2)qR, cyano, amino, mono or di-lower alkyl amino, NHC(O)-lower alkyl, cycloalkyl or is or a five membered heteroaryl, optionally substituted by lower alkyl; wherein R is cyano, di-lower alkyl amino or pyrrolidin-1-yl; R2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; R3 is hydrogen or lower alkyl or CH2OH; R4 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; n is 1, 2 or 3; in case n is 2 or 3, R1 may be the same or different; o is 1, 2 or 3; in case o is 2 or 3, R2 may be the same or different; p is 1, 2 or 3; in case p is 2 or 3, R4 may be the same or different; q is 1 or 2; or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

公开(公告)号：EP2205083A1

公开(公告)日：2010-07-14

申请号：EP08835246.3

申请日：2008-09-30

申请人： Merck Sharp & Dohme Corp. ,  Neuromed Pharmaceuticals Ltd.

发明人： CHAKRAVARTY, Prasun, K. ,  DING, Yanbing ,  DUFFY, Joseph, L. ,  PAJOUHESH, Hassan ,  SHAO, Pengcheng Patrick ,  TYAGARAJAN, Sriram ,  YE, Feng

IPC分类号： A01N43/40 ,  A61K31/445

CPC分类号： C07D211/24 ,  C07D205/04 ,  C07D207/08 ,  C07D211/98 ,  C07D401/06 ,  C07D401/08 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D473/04 ,  C07D487/04

摘要： A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.

公开(公告)号：EP2185540A1

公开(公告)日：2010-05-19

申请号：EP08786547.3

申请日：2008-07-29

申请人： F. Hoffmann-La Roche AG

发明人： JABLONSKI, Philippe ,  KAWASAKI, Kenichi ,  KNUST, Henner ,  LIMBERG, Anja ,  NETTEKOVEN, Matthias ,  RATNI, Hasane ,  RIEMER, Claus ,  WU, Xihan

IPC分类号： C07D401/08 ,  C07D401/06

CPC分类号： C07D401/06 ,  C07D401/08

摘要： The invention relates to a compound of general formula (I) wherein Ar1 is aryl or a five or six membered heteroaryl; Ar2 is aryl or a five or six membered heteroaryl; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, S-lower alkyl, -S(O)2-lower alkyl, -S(O)2-di-lower alkyl amino, -(CH2)qR, cyano, amino, mono or di-lower alkyl amino, NHC(O)-lower alkyl, cycloalkyl or is or a five membered heteroaryl, optionally substituted by lower alkyl; wherein R is cyano, di-lower alkyl amino or pyrrolidin-1-yl; R2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; R3 is hydrogen or lower alkyl or CH2OH; R4 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; n is 1, 2 or 3; in case n is 2 or 3, R1 may be the same or different; o is 1, 2 or 3; in case o is 2 or 3, R2 may be the same or different; p is 1, 2 or 3; in case p is 2 or 3, R4 may be the same or different; q is 1 or 2; or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

摘要翻译： 本发明涉及通式（I）的化合物，其中Ar 1是芳基或五元或六元杂芳基; Ar 2是芳基或五元或六元杂芳基; R1是氢，卤素，低级烷基，低级烷氧基，被卤素取代的低级烷基，被卤素取代的低级烷氧基，S-低级烷基，-S（O）2 - 低级烷基，-S（O）2 - 二低级烷基 氨基， - （CH 2）q R，氰基，氨基，单或二低级烷基氨基，NHC（O） - 低级烷基，环烷基或任选被低级烷基取代的五元杂芳基; 其中R是氰基，二低级烷基氨基或吡咯烷-1-基; R2是氢，卤素，低级烷基，被卤素或氰基取代的低级烷基; R3是氢或低级烷基或CH2OH; R4是氢，卤素，低级烷基，被卤素或氰基取代的低级烷基; n是1,2或3; 在n为2或3的情况下，R1可以相同或不同; o是1,2或3; 在o为2或3的情况下，R2可以相同或不同; p是1,2或3; 在p为2或3的情况下，R 4可以相同或不同; q是1或2; 或其药学活性盐，包括式（I）化合物的所有立体异构形式，单独的非对映异构体和对映异构体以及其外消旋和非外消旋混合物。 已经发现本发明化合物是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意力缺陷多动症（ADHD）的高潜力NK-3受体拮抗剂。